Renzapride
- CAS No.
- 112727-80-7
- Chemical Name:
- Renzapride
- Synonyms
- Renzapride;BRL-24924A;Renzapridum;program AZM-112;4-amino-N-[(4R,5S)-1-azabicyclo[3.3.1]nonan-4-yl]-5-chloro-2-methoxybenzamide;Benzamide, 4-amino-N-(1R,4S,5R)-1-azabicyclo[3.3.1]non-4-yl-5-chloro-2-methoxy-, rel-
- CBNumber:
- CB31075183
- Molecular Formula:
- C16H22ClN3O2
- Molecular Weight:
- 323.82
- MDL Number:
- MFCD00869601
- MOL File:
- 112727-80-7.mol
| Melting point | >260° |
|---|---|
| Boiling point | 469.2±45.0 °C(Predicted) |
| Density | 1.30±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| pka | 13.59±0.20(Predicted) |
| form | Solid |
| color | White to off-white |
| FDA UNII | 9073C0W4E9 |
Renzapride Chemical Properties,Uses,Production
Uses
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist[1]. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study[2].
in vivo
Renzapride (BRL 24924) (100 μg i.v.) results in a partial reverse of both the delayed solid and liquid meals emptying[2].
Renzapride (BRL 24924) (0.5-1 mg/kg) significantly increases the rate of emptying of a 51Cr-labeled liquid meal from the murine stomach[4].
| Animal Model: | Dog (simulating gastroparesis)[2] |
| Dosage: | 100 μg/kg |
| Administration: | i.v. |
| Result: | Results in a partial reverse of both the delayed solid and liquid meals emptying. |
| Animal Model: | Mice (30-45g)[2] |
| Dosage: | 0.5-1 mg/kg |
| Administration: | p.o. |
| Result: | Significantly increase the rate of emptying of a 51Cr-labeled liquid meal from the murine stomach. |
IC 50
5-HT4 Receptor: 115 nM (Ki)
References
[1] Camilleri M, et al. Effect of renzapride on transit in constipation-predominant irritable bowel syndrome. Clin Gastroenterol Hepatol. 2004;2(10):895-904. DOI:10.1016/s1542-3565(04)00391-x
[2] Scarpellini E, et al. Renzapride: a new drug for the treatment of constipation in the irritable bowel syndrome. Expert Opin Investig Drugs. 2008;17(11):1663-1670. DOI:10.1517/13543784.17.11.1663
[3] Nagakura Y, et al. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol Res. 1999;39(5):375-382. DOI:10.1006/phrs.1998.0454
[4] Mawe GM, et al. Blockade of 5-HT-mediated enteric slow EPSPs by BRL 24924: gastrokinetic effects. Am J Physiol. 1989;257(3 Pt 1):G386-G396. DOI:10.1152/ajpgi.1989.257.3.G386
Renzapride Preparation Products And Raw materials
Raw materials
Preparation Products
Renzapride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Shanghai T&W Pharmaceutical Co., Ltd. | +86 21 61551611 | China | 9891 | 58 | |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24739 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D co.,Ltd. | 025-66113011 18112977050 | cb5@aikonchem.com | China | 10359 | 58 |
| mahaloong | +86-028-81192082 +86-18180560816 | sales@mahaloong.com | China | 596 | 58 |
| Sangon Biotech (Shanghai) Co.,Ltd. | 400-821-026 | Sales@sangon.com | China | 48813 | 58 |